| Title: |
Synthesis and biological evaluation of burnettiene A derivatives enabling discovery of novel fungicide candidates. |
| Authors: |
Aoi Kimishima1,2, Atsuka Nishitomi1, Iori Tsuruoka1, Masako Honsho1,2, Sota Negami1, Sota Honma1,2, Katsuyuki Sakai1, Toshiyuki Tokiwa2, Hiroki Kojima1,2, Kenichi Nonaka1,2, Shin-ichi Fuji3, Takumi Chinen4, Takeo Usui4, Yukihiro Asami1,2 yasami@lisci.kitasato-u.ac.jp |
| Source: |
Journal of Pesticide Science. 2024, Vol. 49 Issue 3, p159-167. 9p. |
| Subject Terms: |
*LEPTOSPHAERIA maculans, *RHIZOCTONIA solani, *BOTRYTIS cinerea, *PHYTOPATHOGENIC fungi, *ESTER derivatives, *POLYKETIDES |
| Abstract: |
An antifungal polyene-decalin polyketide natural product, burnettiene A (1) has been re-discovered from the culture broth of Lecanicillium primulinum (current name: Flavocillium primulinum) FKI-6715 strain utilizing our original multidrug-sensitive yeast system. This polyene-decalin polyketide natural product was originally isolated from Aspergillus burnettii. The antifungal activity of 1 against Candida albicans has been reported. However, only one fungal species for the antifungal activity of 1 has been revealed, and details of the antifungal activity against other pathogenic fungus remain unknown. After extensive screening for antifungal activity, we found that 1 exhibits broad antifungal activity against pathogenic plant fungi, including Colletotrichum gloeosporioides, Botrytis cinerea, Pyricularia oryzae, Leptosphaeria maculans, and Rhizoctonia solani. Furthermore, we synthesized 12 derivatives from 1 and evaluated their antifungal activity to reveal the detailed structure--activity relationship. The methyl ester derivative showed antifungal activity against Saccharomyces cerevisiae 12geneΔ0HSR-iERG6 100-fold more potent than that of 1. Our research indicates that 1 would be a promising natural product as a new fungicidal candidate and the methyl ester derivative especially has great potential. [ABSTRACT FROM AUTHOR] |
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| Database: |
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